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Entinostat

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https://www.readbyqxmd.com/read/29391350/overcoming-resistance-to-dna-targeted-agents-by-epigenetic-activation-of-schlafen-11-slfn11-expression-with-class-i-histone-deacetylase-inhibitors
#1
Sai Wen Tang, Anish Thomas, Junko Murai, Jane Trepel, Susan E Bates, Vinodh N Rajapakse, Yves Pommier
PURPOSE: Schlafen 11 (SLFN11), a putative DNA/RNA helicase is a dominant genomic determinant of response to DNA damaging agents and is frequently not expressed in cancer cells. Whether histone deacetylase (HDAC) inhibitors can be used to release SLFN11 and sensitize SLFN11-inactivated cancers to DNA-targeted agents is tested here. EXPERIMENTAL DESIGN: SLFN11 expression was examined in The Cancer Genome Atlas (TCGA), in cancer cell line databases and in patients treated with romidepsin...
February 1, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29354686/e2112-randomized-phase-iii-trial-of-endocrine-therapy-plus-entinostat-placebo-in-patients-with-hormone-receptor-positive-advanced-breast-cancer
#2
REVIEW
Sri Lakshmi Hyndavi Yeruva, Fengmin Zhao, Kathy D Miller, Amye J Tevaarwerk, Lynne I Wagner, Robert J Gray, Joseph A Sparano, Roisin M Connolly
Endocrine therapies are effective in the treatment of hormone receptor (HR)-positive breast cancer, however, de novo or acquired treatment resistance is a significant clinical problem. A potential mechanism of resistance involves changes in gene expression secondary to epigenetic modifications, which might be reversed with the use of histone deacetylase (HDAC) inhibitors such as entinostat. The ENCORE 301 phase II randomized, placebo-controlled study demonstrated a significant improvement in progression-free survival (PFS) and overall survival (OS), with the addition of entinostat to exemestane in patients with HR-positive advanced breast cancer with disease progression after prior non-steroidal aromatase inhibitor (AI)...
2018: NPJ Breast Cancer
https://www.readbyqxmd.com/read/29316653/synergistic-association-of-valproate-and-resveratrol-reduces-brain-injury-in-ischemic-stroke
#3
Lara Faggi, Giuseppe Pignataro, Edoardo Parrella, Vanessa Porrini, Antonio Vinciguerra, Pasquale Cepparulo, Ornella Cuomo, Annamaria Lanzillotta, Mariana Mota, Marina Benarese, Paolo Tonin, Lucio Annunziato, PierFranco Spano, Marina Pizzi
Histone deacetylation, together with altered acetylation of NF-κB/RelA, encompassing the K310 residue acetylation, occur during brain ischemia. By restoring the normal acetylation condition, we previously reported that sub-threshold doses of resveratrol and entinostat (MS-275), respectively, an activator of the AMP-activated kinase (AMPK)-sirtuin 1 pathway and an inhibitor of class I histone deacetylases (HDACs), synergistically elicited neuroprotection in a mouse model of ischemic stroke. To improve the translational power of this approach, we investigated the efficacy of MS-275 replacement with valproate, the antiepileptic drug also reported to be a class I HDAC blocker...
January 6, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29313067/combinatorial-effects-of-histone-deacetylase-inhibitors-hdaci-vorinostat-and-entinostat-and-adaphostin-are-characterized-by-distinct-redox-alterations
#4
Nilsa Rivera-Del Valle, Tiewei Cheng, Mary E Irwin, Hayley Donnella, Melissa M Singh, Joya Chandra
PURPOSE: Amongst the epigenetically targeted therapies, targeting of the histone deacetylases (HDACs) has yielded numerous drugs for clinical use in hematological malignancies, but none as yet for acute lymphocytic leukemia (ALL). Single agent activity of HDAC inhibitors (HDACi) has been elusive in ALL, and has prompted study of combinatorial strategies. Because several HDACi raise levels of intracellular oxidative stress, we evaluated combinations of two structurally distinct HDACi with the redox active compound adaphostin in ALL...
January 8, 2018: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29302039/targeting-the-corest-complex-with-dual-histone-deacetylase-and-demethylase-inhibitors
#5
Jay H Kalin, Muzhou Wu, Andrea V Gomez, Yun Song, Jayanta Das, Dawn Hayward, Nkosi Adejola, Mingxuan Wu, Izabela Panova, Hye Jin Chung, Edward Kim, Holly J Roberts, Justin M Roberts, Polina Prusevich, Jeliazko R Jeliazkov, Shourya S Roy Burman, Louise Fairall, Charles Milano, Abdulkerim Eroglu, Charlotte M Proby, Albena T Dinkova-Kostova, Wayne W Hancock, Jeffrey J Gray, James E Bradner, Sergio Valente, Antonello Mai, Nicole M Anders, Michelle A Rudek, Yong Hu, Byungwoo Ryu, John W R Schwabe, Andrea Mattevi, Rhoda M Alani, Philip A Cole
Here we report corin, a synthetic hybrid agent derived from the class I HDAC inhibitor (entinostat) and an LSD1 inhibitor (tranylcypromine analog). Enzymologic analysis reveals that corin potently targets the CoREST complex and shows more sustained inhibition of CoREST complex HDAC activity compared with entinostat. Cell-based experiments demonstrate that corin exhibits a superior anti-proliferative profile against several melanoma lines and cutaneous squamous cell carcinoma lines compared to its parent monofunctional inhibitors but is less toxic to melanocytes and keratinocytes...
January 4, 2018: Nature Communications
https://www.readbyqxmd.com/read/29298886/class-1-selective-histone-deacetylase-inhibitors-enhance-hiv-latency-reversal-while-preserving-the-activity-of-hdac-isoforms-necessary-for-maximal-hiv-gene-expression
#6
Thomas D Zaikos, Mark M Painter, Nadia T Sebastian, Valeri H Terry, Kathleen L Collins
Combinations of drugs that affect distinct mechanisms of HIV latency aim to induce robust latency reversal leading to cytopathicity and elimination of the persistent HIV reservoir. Thus far, attempts have focused on combinations of PKC agonists and pan-histone deacetylase inhibitors (HDIs) despite the knowledge that HIV gene expression is regulated by class 1 histone deacetylases. We hypothesized that class 1-selective HDIs would promote more robust HIV latency reversal in combination with a PKC agonist than pan-HDIs because they preserve the activity of pro-viral factors regulated by non-class 1 histone deacetylases...
January 3, 2018: Journal of Virology
https://www.readbyqxmd.com/read/29224834/hdac1-localizes-to-the-mitochondria-of-cardiac-myocytes-and-contributes-to-early-cardiac-reperfusion-injury
#7
Daniel J Herr, Mauhamad Baarine, Sverre E Aune, Xiaoyang Li, Lauren E Ball, John J Lemasters, Craig C Beeson, James C Chou, Donald R Menick
RATIONALE: Recent evidence indicates that histone deacetylase enzymes (HDACs) contribute to ischemia reperfusion (I/R) injury, and pan-HDAC inhibitors have been shown to be cardioprotective when administered either before an ischemic insult or during reperfusion. We have shown previously that selective inhibition of class I HDACs provides superior cardioprotection when compared to pan-HDAC inhibition in a pretreatment model, but selective class I HDAC inhibition has not been tested during reperfusion, and specific targets of class I HDACs in I/R injury have not been identified...
December 7, 2017: Journal of Molecular and Cellular Cardiology
https://www.readbyqxmd.com/read/29156837/meta-analysis-of-efficacy-and-adverse-events-of-erlotinib-based-targeted-therapies-for-advanced-metastatic-non-small-cell-lung-cancer
#8
Fei Li, Shu-Hua Zhang, Li-Min Pang
A network meta-analysis evaluating efficacy and adverse events of eight erlotinib-based therapies (erlotinib+placebo, erlotinib+tivantinib, erlotinib+celecoxib, erlotinib+onartuzumab, erlotinib+sunitinib, erlotinib+entinostat, erlotinib+sorafenib, and erlotinib+bevacizumab) for advanced/metastatic non-small-cell lung cancer (NSCLC) was performed. PubMed and Cochrane Library were reviewed, and ten randomized controlled trials were identified in which patients receiving at least one erlotinib-based therapy. Efficacy outcomes, including progression-free survival (PFS), overall survival (OS), overall response rate (ORR), disease control rate (DCR), and adverse outcomes were evaluated...
October 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/29135083/comparison-of-the-anticancer-properties-of-a-novel-valproic-acid-prodrug-to-leading-histone-deacetylase-inhibitors
#9
Nataly Tarasenko, Hanna Chekroun-Setti, Abraham Nudelman, Ada Rephaeli
The HDAC inhibitory activity of valproic acid (VPA) has led to on-going evaluation of it as an anticancer agent. The histone deacetylase (HDAC) inhibitor AN446, a prodrug of VPA, releases the acid upon metabolic degradation. AN446 is >60 fold more potent than VPA in killing cancer cells in vitro. Herein, we compare the activities of AN446, as an anticancer agent, to those of representative types from each of the four major classes of HDAC inhibitors (HDACIs): vorinostat, romidepsin, entinostat and VPA. AN446 exhibited the greatest selectivity and HDAC inhibitory activity against cancer cells...
November 14, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29113455/hdac1-governs-iron-homeostasis-independent-of-histone-deacetylation-in-iron-overload-murine-models
#10
Xiangju Yin, Qian Wu, Jitender Monga, Enjun Xie, Hao Wang, Shufen Wang, Huizhen Zhang, Zhan-You Wang, Tianhua Zhou, Yunjun Shi, Jack Rogers, Hening Lin, Junxia Min, Fudi Wang
AIMS: Iron overload disorders are common and could lead to significant morbidity and mortality worldwide. Due to limited treatment options, there is a great need to develop novel strategies to remove the excess body iron. To discover potential epigenetic modulator in hepcidin upregulation and subsequently decreasing iron burden, we performed an epigenetic screen. The in vivo effects of the identified compounds were further tested in iron-overload mouse models, including Hfe-/-, Hjv-/- and hepatocyte-specific Smad4 knockout (Smad4fl/fl;Alb-Cre+) mice...
November 7, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/29107111/entinostat-reverses-cisplatin-resistance-in-esophageal-squamous-cell-carcinoma-via-down-regulation-of-multidrug-resistance-gene-1
#11
Xiao-Ping Huang, Xuan Li, Min-Yi Situ, Li-Yun Huang, Jun-Ye Wang, Tian-Cheng He, Qi-Hang Yan, Xiu-Ying Xie, Yu-Jing Zhang, Yuan-Hong Gao, Yu-Hong Li, Tie-Hua Rong, Jian-Hua Fu, Qing-Qing Cai, Ming-Rong Wang
Cisplatin resistance frequently occurs in esophageal squamous cell carcinoma (ESCC). The underlying mechanism for cisplatin resistance in ESCC remains largely obscure. Here we report that entinostat reversed cisplatin resistance in ESCC both in vitro and in vivo by induction of apoptosis and inhibition of cell proliferation, accompanied by a decrease of multidrug resistance gene 1 (MDR1), P-Src, Mcl-1, Cyclin D1 and an increase of cleaved PARP. MDR1 expression was associated with worsen survival of ESCC patients with cisplatin-based chemotherapy...
October 26, 2017: Cancer Letters
https://www.readbyqxmd.com/read/29039546/antiproliferative-effects-of-tsa-pxd%C3%A2-101-and-ms%C3%A2-275-in-a2780-and-mcf7-cells-acetylated-histone-h4-and-acetylated-tubulin-as-markers-for-hdaci-potency-and-selectivity
#12
Vasilis P Androutsopoulos, Demetrios A Spandidos
Inhibition of histone deacetylase enzymes (HDACs) has been well documented as an attractive target for the development of chemotherapeutic drugs. The present study investigated the effects of two prototype hydroxamic acid HDAC inhibitors, namely Trichostatin A (TSA) and Belinostat (PXD‑101) and the benzamide Entinostat (MS‑275) in A2780 ovarian carcinoma and MCF7 breast adenocarcinoma cells. The three HDACi inhibited the proliferation of A2780 and MCF7 cells at comparable levels, below the µM range. Enzyme inhibition assays in a cell‑free system showed that TSA was the most potent inhibitor of total HDAC enzyme activity followed by PXD‑101 and MS‑275...
October 6, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28969017/use-of-a-genome-wide-haploid-genetic-screen-to-identify-treatment-predicting-factors-a-proof-of-principle-study-in-pancreatic-cancer
#13
Yuk Ting Ma, Sarah M Leonard, Naheema Gordon, Jennifer Anderton, Claire James, David Huen, Ciaran B Woodman, Daniel H Palmer
The ability to develop a comprehensive panel of treatment predicting factors would significantly improve our ability to stratify patients for cytotoxic or targeted therapies, and prevent patients receiving ineffective treatments. We have investigated if a recently developed genome-wide haploid genetic screen can be used to reveal the critical mediators of response to anticancer therapy. Pancreatic cancer is known to be highly resistant to systemic therapy. Recently epigenetic changes have been shown to be a key determinant in the maintenance of subpopulations of cancer cells with high-level resistance to cytotoxic therapy...
September 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28952409/targeting-triple-negative-breast-cancer-with-histone-deacetylase-inhibitors
#14
REVIEW
Palma Fedele, Laura Orlando, Saverio Cinieri
Triple negative breast cancer (TNBC) is a heterogeneous disease characterized by poor outcomes, higher rates of relapse, lack of biomarkers for rational use of targeted treatments and insensitivity to current available treatments. Histone deacetylase inhibitors (HDACis) perform multiple cytotoxic actions and are emerging as promising multifunctional agents in TNBC. Areas covered: This review focuses on the challenges so far addressed in the targeted treatment of TNBC and explores the various mechanisms by which HDACis control cancer cell growth, tumor progression and metastases...
November 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28939740/immunomodulation-by-entinostat-in-renal-cell-carcinoma-patients-receiving-high-dose-interleukin-2-a-multicenter-single-arm-phase-1-2-trial-nci-ctep-7870
#15
Roberto Pili, David I Quinn, Hans Hammers, J Paul Monk, Saby George, Tanya Dorff, Thomas Olencki, Li Shen, Ashley R Orillion, Dominick Lamonica, Roberto A Salas Fragomeni, Zsolt Szabo, Alan D Hutson, Adrienne Groman, Susan M Perkins, Richard L Piekarz, Michael A Carducci
PURPOSE: Based on preclinical data suggesting that the class I selective HDAC inhibitor entinostat exerts a synergistic antitumor effect in combination with high dose interleukin 2 (IL-2) in a renal cell carcinoma model by down-regulating Foxp3 expression and function of regulatory T cells (Treg), we conducted a phase I/II clinical study with entinostat and high dose IL-2 in patients with metastatic clear cell renal cell carcinoma (ccRCC). EXPERIMENTAL DESIGN: Clear cell histology, no prior treatments, and being sufficiently fit to receive high dose IL-2 were the main eligibility criteria...
September 22, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28919994/effect-of-entinostat-on-nk-cell-mediated-cytotoxicity-against-osteosarcoma-cells-and-osteosarcoma-lung-metastasis
#16
Simin Kiany, Gangxiong Huang, Eugenie S Kleinerman
There is a crucial need for a new therapeutic approach for osteosarcoma (OS) lung metastasis since this disease remains the main cause of mortality in OS. We previously demonstrated that natural killer (NK) cell therapy has minimal efficacy against OS metastasis. This study determined whether the histone deacetylase inhibitor entinostat could immunosensitize OS cells to NK cell lysis and increases the efficacy of NK cell therapy for OS lung metastasis. Entinostat upregulated ligands for NK cell-activating receptors (major histocompatibility complex [MHC] class I polypeptide-related chain A [MICA] and B [MICB]; UL16 binding proteins 1, 2, 5, and 6; and CD155) on OS cells both in vitro and in vivo and led to more susceptibility to NK cell-mediated cytotoxicity in vitro...
2017: Oncoimmunology
https://www.readbyqxmd.com/read/28870998/histone-deacetylases-as-new-therapeutic-targets-in-triple-negative-breast-cancer-progress-and-promises
#17
REVIEW
Nikolaos Garmpis, Christos Damaskos, Anna Garmpi, Emmanouil Kalampokas, Theodoros Kalampokas, Eleftherios Spartalis, Afrodite Daskalopoulou, Serena Valsami, Michael Kontos, Afroditi Nonni, Konstantinos Kontzoglou, Despina Perrea, Nikolaos Nikiteas, Dimitrios Dimitroulis
Triple-negative breast cancer (TNBC) lacks expression of estrogen receptor (ER), progesterone receptor (PR) and HER2 gene. It comprises approximately 15-20% of breast cancers (BCs). Unfortunately, TNBC's treatment continues to be a clinical problem because of its relatively poor prognosis, its aggressiveness and the lack of targeted therapies, leaving chemotherapy as the mainstay of treatment. It is essential to find new therapies against TNBC, in order to surpass the resistance and the invasiveness of already existing therapies...
September 2017: Cancer Genomics & Proteomics
https://www.readbyqxmd.com/read/28840475/histone-deacetylase-inhibitor-entinostat-ms-275-restores-anesthesia-induced-alteration-of-inhibitory-synaptic-transmission-in-the-developing-rat-hippocampus
#18
Srdjan M Joksimovic, Hari Prasad Osuru, Azra Oklopcic, Mark P Beenhakker, Vesna Jevtovic-Todorovic, Slobodan M Todorovic
Recent evidence strongly supports the idea that common general anesthetics (GAs) such as isoflurane (Iso) and nitrous oxide (N2O; laughing gas), as well as sedative drugs such as midazolam are neurotoxic for the developing mammalian brain having deleterious effects on neural circuits involved in cognition, learning and memory. However, to date, very little is known about epigenetic mechanisms involved in GA-induced plasticity of synaptic transmission in the hippocampus, the main memory-processing region in the brain...
August 24, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28738707/clinical-evaluation-of-combined-azacitidine-and-entinostat-on-the-induction-of-fetal-hemoglobin-in-patients-with-acute-myeloid-leukemias-and-myelodysplastic-syndromes
#19
Katharine R Press, Natalie Uy, Jeffrey Keefer, Steven D Gore, Hetty E Carraway, Sarah Sakoian, Thomas Prebet
No abstract text is available yet for this article.
July 25, 2017: Leukemia & Lymphoma
https://www.readbyqxmd.com/read/28733542/use-of-a-genome-wide-haploid-genetic-screen-to-identify-treatment-predicting-factors-a-proof-of-principle-study-in-pancreatic-cancer
#20
Yuk Ting Ma, Sarah M Leonard, Naheema Gordon, Jennifer Anderton, Claire James, David Huen, Ciaran B Woodman, Daniel H Palmer
The ability to develop a comprehensive panel of treatment predicting factors would significantly improve our ability to stratify patients for cytotoxic or targeted therapies, and prevent patients receiving ineffective treatments. We have investigated if a recently developed genome-wide haploid genetic screen can be used to reveal the critical mediators of response to anticancer therapy. Pancreatic cancer is known to be highly resistant to systemic therapy. Recently epigenetic changes have been shown to be a key determinant in the maintenance of subpopulations of cancer cells with high-level resistance to cytotoxic therapy...
June 29, 2017: Oncotarget
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